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1.
Dis Aquat Organ ; 137(3): 175-183, 2020 Jan 16.
Artigo em Inglês | MEDLINE | ID: mdl-31942863

RESUMO

Flavobacterial infections are among the causes of fish losses in farms with the emergence of antibiotic-resistant isolates. Silver nanoparticles (AgNPs) are known for their potent antimicrobial activity against different types of bacteria. In this study, we evaluated the antibacterial properties of AgNPs (diameter: 23 nm) against Flavobacterium johnsoniae infection in common carp Cyprinus carpio. The assays included both in vitro and in vivo antibacterial tests in addition to evaluation of cell toxicity effects on the fish cell lines. The in vitro results revealed potent inhibitory effects of AgNPs on the growth of F. johnsoniae with a minimum inhibitory concentration of 34 µg ml-1. Fish cell (epithelioma papulosum cyprini and koi carp fin) viability was 95-100% after exposure to 500 ng ml-1 (and lower concentrations) of AgNPs. In the exposure experiment, mortality rates decreased from 45% in the infected non-treated group to 30 and 15% in the intraperitoneal injection and immersion-treated groups, respectively. Neither of the treated groups showed any clinical signs or histopathological lesions. The single-dose treatment with AgNPs during early infection with F. johnsoniae aided in minimizing fish losses.


Assuntos
Carpas , Nanopartículas Metálicas , Animais , Flavobacterium , Testes de Sensibilidade Microbiana , Prata
2.
Int J Clin Pharmacol Ther ; 58(1): 50-56, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31670654

RESUMO

OBJECTIVE: Patients with cerebral hemorrhage are often prone to intracranial infection, and meropenem is recommended for treatment. But whether the widely used dosing regimen (1 g, 2-hour infusion, every 12 hours) is suitable for antibiotic therapy is still unclear. The purpose of this study was to perform pharmacokinetic/pharmacodynamic (PK/PD) analyses of meropenem in both plasma and cerebrospinal fluid (CSF) in these patients. MATERIALS AND METHODS: Ten patients were enrolled in the present study. The blood samples and CSF samples were taken at predetermined time points and determined by our previously developed HPLC method. Pharmacokinetic parameters were then calculated, and the probability of target attainment (PTA) was calculated by the time that drug concentrations were above the minimum inhibitory concentration (%T>MIC). RESULTS: The peak meropenem concentration (Cmax) of 17.79 ± 3.38 µg/mL in plasma was reached at 2 hours, and the area under the curve (AUC) was 46.95 ± 4.37 h×µg/mL. The Cmax of 6.51 ± 1.11 µg/mL in CSF was reached at 3.50 ± 0.53 hours, and the AUC was 24.53 ± 4.28 h×µg/mL. The average penetration rate of meropenem in these patients was 52.25%. In the case where the MIC value was ≤ 1 µg/mL and using 40%T>MIC as a PK/PD index, the PTA of meropenem in both plasma and CSF were able to provide good coverage with MIC ≤ 1 µg/mL. CONCLUSION: In conclusion, this is the first study on the PK/PD analysis of meropenem in both plasma and CSF in patients with cerebral hemorrhage. The results will assist in selecting appropriate dosing regimens of meropenem in these patients.


Assuntos
Antibacterianos/farmacocinética , Hemorragia Cerebral , Drenagem , Meropeném/farmacocinética , Antibacterianos/sangue , Antibacterianos/líquido cefalorraquidiano , Humanos , Meropeném/sangue , Meropeném/líquido cefalorraquidiano , Testes de Sensibilidade Microbiana , Método de Monte Carlo
3.
Fitoterapia ; 140: 104406, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31698061

RESUMO

One new quinoline alkaloid (1), two new bisabolane-type sesquiterpene derivatives (2 and 3), and a new natural product (4) along with ten known compounds (514) were isolated from the deep sea-derived fungus Aspergillus sp. SCSIO06786 which cultured on solid rice medium. Three new structures were elucidated by analysis of 1D/2D NMR data and HR-ESI-MS. The absolute configurations of 2 and 3 were established by comparison of the experimental and reported ECD values. Compounds 11-13 exhibited moderate selective inhibitory activities against the tested pathogenic bacteria with MIC values among 3.13-12.5 µg/mL.


Assuntos
Alcaloides/isolamento & purificação , Aspergillus/química , Quinolinas/isolamento & purificação , Água do Mar/microbiologia , Sesquiterpenos/isolamento & purificação , Alcaloides/farmacologia , Antibacterianos/isolamento & purificação , Antibacterianos/farmacologia , Bactérias/efeitos dos fármacos , Sedimentos Geológicos/microbiologia , Oceano Índico , Testes de Sensibilidade Microbiana , Estrutura Molecular , Quinolinas/farmacologia , Sesquiterpenos/farmacologia
4.
Chem Pharm Bull (Tokyo) ; 68(1): 64-69, 2020 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-31708557

RESUMO

Invasive fungal disease constitutes a growing health problem and development of novel antifungal drugs with high potency and selectivity are in an urgent need. In this study, a novel series of triazole derivatives containing different ester skeleton were designed and synthesized. Microdilution broth method was used to investigate antifungal activity. Significant inhibitory activity of compounds 5c, 5d, 5e, 5f, 5m and 5n was evaluated against the Candida albicans (I), Candida albicans clinical isolate (II), Candida glabrata clinical isolate (I), and Candida glabrata (II) with minimum inhibitory concentrations (MIC80) values ranging from 2 to 16 µg/mL. Notably, compounds 5e and 5n showed the best inhibition against Candida albicans (II), Candida glabrata (I), and Candida glabrata (II) at the concentrations of 2 and 8 µg/mL, respectively. Molecular docking study revealed that the target compounds interacted with CYP51 mainly through hydrophobic and van der Waals interactions. The results indicated that these novel triazole derivatives could serve as promising leads for development of antifungal agents.


Assuntos
Antifúngicos/síntese química , Desenho de Drogas , Simulação de Acoplamento Molecular , Triazóis/química , Antifúngicos/química , Antifúngicos/farmacologia , Sítios de Ligação , Candida/efeitos dos fármacos , Domínio Catalítico , Ésteres/química , Testes de Sensibilidade Microbiana , Eletricidade Estática , Esterol 14-Desmetilase/química , Esterol 14-Desmetilase/metabolismo , Relação Estrutura-Atividade , Triazóis/síntese química , Triazóis/farmacologia
5.
Fitoterapia ; 140: 104422, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31756377

RESUMO

Peniterester (1), a new tricyclic sesquiterpene, together with 6 known compounds (2-7) were isolated from the secondary metabolites of an artificial mutant Penicillium sp. T2-M20 which was obtained from the parental strain Penicillium sp. T2-8 via UV irradiation as well as nitrosoguanidine (NTG) induction. Peniterester was only produced by the mutant T2-M20 on the basis of LC-MS analysis. Meanwhile, the results of in vitro bioactivities screening indicated that peniterester owned obvious antibacterial activities against Bacillus subtilis, Escherichia coli and Staphylococcus aureus with MICs of 8.0, 8.0 and 4.0 µg/mL, respectively.


Assuntos
Antibacterianos/farmacologia , Penicillium/química , Sesquiterpenos/farmacologia , Antibacterianos/isolamento & purificação , Bacillus subtilis/efeitos dos fármacos , Linhagem Celular Tumoral , China , Escherichia coli/efeitos dos fármacos , Gastrodia/microbiologia , Humanos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Rizoma/microbiologia , Metabolismo Secundário , Sesquiterpenos/isolamento & purificação , Staphylococcus aureus/efeitos dos fármacos
6.
Chem Commun (Camb) ; 56(3): 356-359, 2020 Jan 02.
Artigo em Inglês | MEDLINE | ID: mdl-31825398

RESUMO

A facile and scalable strategy for the quick library synthesis of linear-, hinged-, star-, and cyclic-polypeptides with broad-spectrum antimicrobial activity has been reported. The topologically nanoengineered polypeptides show superior antimicrobial activity against Gram-positive and Gram-negative bacteria and low toxicity, allowing screening of architectural polypeptides as mimics of host defense peptides for antimicrobials.


Assuntos
Anti-Infecciosos/síntese química , Peptídeos/química , Animais , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Camundongos , Testes de Sensibilidade Microbiana , Microscopia Confocal , Células NIH 3T3 , Nanotecnologia , Peptídeos/síntese química , Peptídeos/farmacologia
7.
J Sci Food Agric ; 100(1): 335-342, 2020 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-31584691

RESUMO

BACKGROUND: Antibacterial activity of honey is not only crucial characteristic in selection of honey for medical usage but also an important honey quality marker. The aim of the study was to characterise the antibacterial potential of 29 honey samples representing the main types of multi-floral blossom and honeydew honeys produced in Switzerland. Antibacterial activity against Staphylococcus aureus and Pseudomonas aeruginosa was expressed as a minimum inhibitory and bactericidal concentrations (MIC and MBC). Furthermore, the content of bee-derived glucose oxidase (GOX) and its enzymatic product, H2 O2 , were also evaluated. RESULTS: All honey samples successfully met basic defined criteria (moisture and hydroxymethylfurfural (HMF)) tested in this study. Honeydew honeys were the most effective honey samples and generated the highest levels of H2 O2 . A strong significant correlation was found between the overall antibacterial activity and the level of H2 O2 among all honey samples. Interestingly, the content of GOX in honey samples did not correlate with their antibacterial activity as well as H2 O2 production capacity. A weak antibacterial activity was determined in five floral honeys, most likely due to increased enzymatic activity of pollen-derived catalase. CONCLUSION: This study showed that antibacterial effect of Swiss honey samples is associated mainly with H2 O2 . © 2019 Society of Chemical Industry.


Assuntos
Antibacterianos/análise , Mel/análise , Animais , Antibacterianos/farmacologia , Abelhas , Catalase/análise , Glucose Oxidase/análise , Mel/classificação , Testes de Sensibilidade Microbiana , Pseudomonas aeruginosa/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos , Suíça
8.
Arch Oral Biol ; 109: 104577, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31606567

RESUMO

Although the effectiveness of some mouthwashes has been proven, phytotherapy is still a field to be explored as an alternative to commercial products. OBJECTIVE: To evaluate, in vitro, the cytotoxicity and efficacy of two solutions based on citronella oil (CN), on S. aureus and C. albicans biofilms (in formation-adhesion phase and 24 h-biofilm formation) on acrylic resin and nickel-chromium alloy samples (one trademark of each material), compared to two alcohol-free commercial mouthwashes. MATERIAL AND METHODS: Two solutions containing CN at concentrations of 5x and 10x the minimum bactericidal/fungicidal concentration (MBC/MFC) were prepared by microdilution. After contamination of the samples surfaces with these microorganisms, the mouthwashes (CN - 5x and 10x; CHX - 0,12% alcohol-free chlorhexidine and LT - alcohol-free essential oils) were evaluated. Mouthwash simulation was performed for 1 min at two moments, the first simulation after 4 h of microbial adhesion and 24 h-biofilm formation, and the second simulation, 6 h after the first simulation. For biofilm quantification, the number of cultured cells was evaluated by CFUs. The cytotoxicity assay was performed on HaCat epithelial cells and quantified by the MTT method. RESULTS: Tested solutions completely inhibited the growth of both microorganisms in the adhesion phase. All solutions showed inhibitory activity against 24 h-biofilm formation. However, CN led to greater microbial reduction, regardless of the surface of the sample. All solutions demonstrated a toxic effect. However, after serial dilution, CN presented the lowest cytotoxic effect. CONCLUSION: Citronella had a lower cytotoxic effect and a higher action compared to commercial solutions.


Assuntos
Biofilmes/efeitos dos fármacos , Cymbopogon/química , Prótese Dentária/microbiologia , Antissépticos Bucais/farmacologia , Óleos Vegetais/farmacologia , Anti-Infecciosos/farmacologia , Candida albicans/efeitos dos fármacos , Linhagem Celular , Humanos , Testes de Sensibilidade Microbiana , Staphylococcus aureus/efeitos dos fármacos
9.
APMIS ; 128(1): 25-34, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31628820

RESUMO

Eradication failure of Helicobacter pylori infection could play a causal role in progression of gastric disorders. In this study, infection with H. pylori was followed in gastric biopsies of symptomatic adult patients at two phases during 1-year period. Analyses were done to show association of therapeutic regimens with the refractory infection, changes in sequence types (STs) and minimum inhibitory concentration (MIC) values, and progression of histopathological changes. Infection with H. pylori was confirmed in 32.3% (57/170) of the patients. Persistent infection with H. pylori was confirmed in 14 out of the 25 patients (56%) who participated at the second phase of the study. A difference between primary and secondary resistance rates to clarithromycin (49% vs 64.3%), metronidazole (76.36% vs 100%), and ciprofloxacin (45% vs 57.1%) was detected. Although the re-emerged strains in patients with refractory infection did not show alteration in STs, their MIC50 values showed twofold increases for clarithromycin and ciprofloxacin. While ciprofloxacin containing regimens were more successful, failure of metronidazole containing regimens was detected in 77% of the patients. Consequently, inappropriate medication has an impact on refractory H. pylori infection, which could cause to a rise in resistance levels to antibiotics and progression of pathological disorders.


Assuntos
Antibacterianos/uso terapêutico , Farmacorresistência Bacteriana Múltipla , Infecções por Helicobacter/tratamento farmacológico , Infecções por Helicobacter/patologia , Helicobacter pylori/efeitos dos fármacos , Idoso , Idoso de 80 Anos ou mais , Antibacterianos/farmacologia , Técnicas de Tipagem Bacteriana , Biópsia , Ciprofloxacino/farmacologia , Claritromicina/farmacologia , Feminino , Seguimentos , Técnicas Histológicas , Humanos , Concentração Inibidora 50 , Masculino , Testes de Sensibilidade Microbiana , Pessoa de Meia-Idade , Tipagem de Sequências Multilocus , Estômago/microbiologia , Estômago/patologia
10.
APMIS ; 128(1): 20-24, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31630449

RESUMO

A case of bacteremia with the fastidious bacteria Actinomyces urogenitalis following lengthy urinary retention is reported in a sixty-year-old man. In 2013, the first case of bacteremia due to A. urogenitalis was presented, secondary to a tubo-ovarian abscess following transvaginal oocyte retrieval. To the best of our knowledge, this is the first male bacteremic episode involving A. urogenitalis related to a urinary tract focus. The patient had no prior urogenital medical history. Extensive susceptibility testing was done on isolates from urinary and blood cultures. The organism exhibited fluoroquinolone resistance but was susceptible to most other antibiotics used in the treatment of urinary infections. Due to its unusual growth requirements infections with A. urogenitalis are most likely an underdiagnosed entity.


Assuntos
Actinomicose/diagnóstico , Bacteriemia/microbiologia , Retenção Urinária/complicações , Infecções Urinárias/microbiologia , Actinomyces , Antibacterianos/uso terapêutico , Bacteriemia/tratamento farmacológico , Farmacorresistência Bacteriana , Humanos , Masculino , Testes de Sensibilidade Microbiana , Pessoa de Meia-Idade , Resultado do Tratamento
11.
Biosci Biotechnol Biochem ; 84(1): 143-153, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31549575

RESUMO

Brevinin-GR23 (B-GR23) was a brevinin-2 like antimicrobial peptide, which had antimicrobial activity against Staphylococcus aureus with minimum inhibitory concentration (MIC) of 16 µM. B-GR23 increased the bacterial membrane permeation, leading to the damage of membrane integrity and the leakage of genomic DNA, then causing the cell death. The peptide nearly inhibited all plantonic bacteria to start the initial attachment of biofilm at the concentration of 1 × MIC. Whereas the disruption rates on immature and mature biofilm decreased from 60% to 20%. B-GR23 reduced the production of extracellular polysaccharides (EPS) in the planktonic growth of S. aureus, which is a crucial structure of biofilm formation. B-GR23 with the concentration of ½ × MIC inhibited 50% water-soluble EPS, and 48% water-insoluble EPS, which contributed to the antibiofilm activity. B-GR23 had no significant toxicity to human blood cells under-tested concentration (200 µM), making it a potential template for designing antimicrobial peptides.


Assuntos
Proteínas de Anfíbios/farmacologia , Antibacterianos/farmacologia , Peptídeos Catiônicos Antimicrobianos/farmacologia , Biofilmes/efeitos dos fármacos , Staphylococcus aureus/fisiologia , Animais , Antibacterianos/síntese química , Peptídeos Catiônicos Antimicrobianos/síntese química , Peptídeos Catiônicos Antimicrobianos/química , Permeabilidade da Membrana Celular/efeitos dos fármacos , DNA Bacteriano/efeitos dos fármacos , DNA Bacteriano/metabolismo , Eritrócitos/efeitos dos fármacos , Hemólise/efeitos dos fármacos , Temperatura Alta , Humanos , Concentração de Íons de Hidrogênio , Testes de Sensibilidade Microbiana/métodos , Polissacarídeos Bacterianos/antagonistas & inibidores , Conformação Proteica em alfa-Hélice , Estabilidade Proteica/efeitos da radiação , Ranidae , Infecções Estafilocócicas/tratamento farmacológico
12.
APMIS ; 128(1): 41-47, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31692136

RESUMO

Campylobacteriosis is one of the most frequently reported zoonoses worldwide. The well-documented increase in the ciprofloxacin resistance has increased the importance of rapid detection of the resistance. The incidence of ciprofloxacin resistance was investigated using real-time PCR. Identification of one hundred and fifty-eight strains was performed by PCR. Minimum inhibitory concentration (MIC) of ciprofloxacin was determined by Epsilometer test. Following the confirmation of the efficiencies of singleplex real-time PCR methods using two different probes, a cytosine to thymine point mutation at codon 86 was detected by allelic discrimination. Of the 158 strains, 114 (72.2%) were determined to be resistant to ciprofloxacin. The MIC50 and the MIC90 of ciprofloxacin were found to be 8 and ≥32 mg/L, respectively. By real-time PCR, the presence of the mutation was confirmed in all, but one, resistant strains and the absence of the mutation was demonstrated in all, but one, susceptible strains. The rate of resistance is high among C. jejuni strains and ciprofloxacin should not be used in the treatment of such infections in Turkey. A cytosine to thymine mutation is the most frequently detected mechanism for the resistance. Real-time PCR can be used for the quick screening of the resistance.


Assuntos
Antibacterianos/farmacologia , Campylobacter jejuni/efeitos dos fármacos , Campylobacter jejuni/genética , Ciprofloxacino/farmacologia , Farmacorresistência Bacteriana/genética , Mutação Puntual , Alelos , Infecções por Campylobacter/epidemiologia , Infecções por Campylobacter/microbiologia , Testes de Sensibilidade a Antimicrobianos por Disco-Difusão , Eletroforese em Gel de Campo Pulsado , Humanos , Concentração Inibidora 50 , Testes de Sensibilidade Microbiana , Fenótipo , Prevalência , Turquia
13.
J Colloid Interface Sci ; 558: 47-54, 2020 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-31580954

RESUMO

The unique antibacterial characteristics of Ag nanomaterials offer a wide potential range of applications, but achieving rapid and durable antibacterial efficacy is challenging. This is because the speed and durability of the antibacterial function make conflicting demands on the structural design: the former requires the direct exposure of Ag to the surrounding environment, whereas the durability requires Ag to be protected from the environment. To overcome this incompatibility, we synthesize sandwich-structured polydopamine shells decorated both internally and externally with Ag nanoparticles, which exhibit prompt and lasting bioactivity in applications. These shells are biocompatible and can be used in vivo to counter bacterial infection caused by methicillin-resistant Staphylococcus aureus superbugs and to inhibit biofilm formation. This work represents a new paradigm for the design of composite materials with enhanced antibacterial properties.


Assuntos
Antibacterianos/química , Materiais Biocompatíveis/química , Indóis/química , Nanopartículas Metálicas/química , Polímeros/química , Prata/química , Animais , Antibacterianos/farmacologia , Materiais Biocompatíveis/farmacologia , Escherichia coli/efeitos dos fármacos , Humanos , Masculino , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Ratos , Ratos Sprague-Dawley
14.
Zhonghua Liu Xing Bing Xue Za Zhi ; 40(11): 1403-1408, 2019 Nov 10.
Artigo em Chinês | MEDLINE | ID: mdl-31838812

RESUMO

Objective: To investigate the molecular characterization of adult diarrhea cases caused by enterotoxic Escherichia coli (ETEC) and explore the practical model of epidemiology for laboratory technique and data needs based on the surveillance network. Methods: Epidemiological design and sampling targeted adult cases ETEC caused diarrhea in epidemic season. The enterotoxin type, serogroup, resistance, colonization factor and molecular type of ETEC were identified. Multiple dynamic phenotypic characteristics of ETEC were indicated by multidimensional and multivariable data. Results: From 2016 to 2018, 84 eligible ETEC strains were detected. The dominant serums/toxins were O∶6 (STh), O∶25 (LT), O∶159 (STh), O∶153 (STh). O∶6 (STh+CS21), which replaced O∶25 and O∶159 as the popular clones in 2018. Six cases of O∶153 (STh+CFA/I+CS8+PT34) in outbreak in 2017 were imported ones. The resistance rates of ETEC strains detected in adults to sulfasoxazole, naproxinic acid, ampicillin and azithromycin were more than 30%, multidrug resistance (MDR) reached 58.3%. Serum/toxin types suggested that attenuated strains were more likely to become MDR. Molecular typing confirmed that the genetic similarity of the dominant clone of O∶6 serogroup (PT20-24) was higher than O∶25 and O∶159. There was a high correlation between the minimal inhibitory concentration (MIC) of azithromycin and the resistant gene mphA (87.5%, 28/32). O∶6 (STh+CS21+mphA) resistant clone was first detected in 2016. Conclusion: A new epidemic clone in adult ETEC diarrhea cases in Shanghai was O∶6 (STh+CS21+mphA). For the first time the association between azithromycin resistance gene mphA and a serum group of ETEC was observed. Multidimensional and multivariate analysis techniques based on epidemiology can help reveal the potential transmission pattern of ETEC for the accurate surveillance and early warning of outbreaks.


Assuntos
Antibacterianos/farmacologia , Azitromicina/uso terapêutico , Diarreia/tratamento farmacológico , Escherichia coli Enterotoxigênica/genética , Escherichia coli Enterotoxigênica/isolamento & purificação , Enterotoxinas/análise , Infecções por Escherichia coli/tratamento farmacológico , Infecções por Escherichia coli/microbiologia , Adulto , China , Diarreia/microbiologia , Resistência Microbiana a Medicamentos , Escherichia coli Enterotoxigênica/classificação , Escherichia coli Enterotoxigênica/efeitos dos fármacos , Enterotoxinas/genética , Proteínas de Escherichia coli/genética , Humanos , Testes de Sensibilidade Microbiana , Sorogrupo , Sorotipagem
15.
Zhongguo Shi Yan Xue Ye Xue Za Zhi ; 27(6): 1774-1778, 2019 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-31839037

RESUMO

OBJECTIVE: To investigate the clinical characteristics, etiology and drug susceptibility of bacterial bloodstream infections in acute leukemia(AL) patients. METHODS: Clinical data, etiology and drug susceptibility of acute leukemia patients with bacterial bloodstream infections from April 2009 to April 2018 were retrospectively analyzed. RESULTS: A total of 376 strains were isolated, 76.9% was Gram-negative bacterial and 23.1% was Gram-positive bacteria. Escherichia coli, Pseudomonas aeruginosa and Klebsiella pneumoniae were listed as the top three of Gram-negative bacteria. The susceptibility of Escherichia coli to the tigacycline, imipenem and meropenem was 100.0%, 98.2% and 98.1%, respectively. The susceptibility of Klebsiella pneumoniae to the tigacycline, imipenem and meropenem were 100.0%, 98.3% and 94.4%, respectively. The adjustment rate for initial use of carbopenems was 3.8%, while the adjustment rate for initial use of noncarbopenems was 74.3% in patients with main Gram-negative bacterial blood stream infection. The susceptibility of Gram-positive bacteria to glycopeptide antibiotics, linezolid and tigacycline was 100.0%. CONCLUSION: Gram-negative bacteria is the majority type of bacteria in AL patients with bacteria blood stream infections. The susceptibility of Gram-negative bacteria to the carbapenems is high, and the treatment adjustment rate is obviously low. The glycopeptide, linezolid and tigacycline are effective for Gram-positive bacteria infections..


Assuntos
Bacteriemia , Bactérias Gram-Negativas , Bactérias Gram-Positivas , Humanos , Testes de Sensibilidade Microbiana , Estudos Retrospectivos
16.
Zhongguo Shi Yan Xue Ye Xue Za Zhi ; 27(6): 1825-1830, 2019 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-31839045

RESUMO

OBJECTIVE: To analyze the risk factors affecting the chemotherapy-related infections in patients with acute lympho-blastic leukemia (ALL). METHODS: The clinical data of 102 patients with ALL from January 2014 to December 2018 were collected and retrospectively studies. The risk factors of chemotherapy-related infections were analyzed by univa-riate and multivariate logistic regression. RESULTS: A total of 386 courses of chemotherapy were completed, out of which the infection occurred in 201 course, with the infection rate of 52.07%, identified infection number was 215 case-times, including perianal infection of 13.95% (30/215), oral infection of 13.49% (29/215), blood flow infection of 1721% (37/215), lower respiratory tract infection of 37.21% (80/215), urinary infection of 3.26% (7/215), skin infection of 3.72% (8/215), digestive and intra abdominal infection of 9.30% (20/215), and other infections of 1.86 (4/215). Totally 88 strains of pathogenic bacteria were detected, including 29 Gram-positive bacteria (32.95%), 52 Gram-negative bacteria (59.09%) and 7 fungi (7.95%). Gram-positive bacteria mainly were Staphylococcus haemolyticus and Enterococcus faecium, susceptible to tegacycline, vancomycin and linezolid; Gram-negative bacteria mainly were Pseudomonas aeruginosa, Escherichia coli and Klebsiella pneumoniae, susceptible to tegacycline, amikacin, piperacillin/tazobactam and imipenem; Candida was the dominant fungus. Living in an ordinart ward, neutrophil defi-ciency for more than 7 days after chemotherapy and incomplete remission were independent risk factors of related infections during the induction chemotherapy in ALL inpatients, and hospitalization time also closely related with chemo-therapy-related infections in ALL inpatients (P<0.05). Neutrophil deficiency for more than 7 days after chemotherapy was an independent risk factor of chemotherapy-related infections in ALL inpatients in the consolidation chemotherapy (P<0.05). CONCLUSION: Patients with ALL are prone to chemotherapeutic-related infections, and those who lack neutrophils for more than 7 days after chemotherapy and who do not reach complete remission are more prone to infection. Living in laminar flow ward and reducing hospitalization stay can help reduce the incidence of infection.


Assuntos
Leucemia-Linfoma Linfoblástico de Células Precursoras , Farmacorresistência Bacteriana , Bactérias Gram-Negativas , Humanos , Testes de Sensibilidade Microbiana , Estudos Retrospectivos , Fatores de Risco
17.
J Enzyme Inhib Med Chem ; 34(1): 1730-1739, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31822127

RESUMO

A series of readily accessible 1-(piperidin-3-yl)thymine amides was designed, synthesised and evaluated as Mycobacterium tuberculosis TMPK (MtbTMPK) inhibitors. In line with the modelling results, most inhibitors showed reasonable MtbTMPK inhibitory activity. Compounds 4b and 4i were slightly more potent than the parent compound 3. Moreover, contrary to the latter, amide analogue 4g was active against the avirulent M. tuberculosis H37Ra strain (MIC50=35 µM). This finding opens avenues for future modifications.


Assuntos
Amidas/farmacologia , Antituberculosos/farmacologia , Inibidores Enzimáticos/farmacologia , Mycobacterium tuberculosis/efeitos dos fármacos , Núcleosídeo-Fosfato Quinase/antagonistas & inibidores , Timina/farmacologia , Amidas/síntese química , Amidas/química , Antituberculosos/síntese química , Antituberculosos/química , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/química , Testes de Sensibilidade Microbiana , Estrutura Molecular , Mycobacterium tuberculosis/enzimologia , Núcleosídeo-Fosfato Quinase/metabolismo , Relação Estrutura-Atividade , Timina/síntese química , Timina/química
18.
BMC Infect Dis ; 19(1): 1040, 2019 Dec 10.
Artigo em Inglês | MEDLINE | ID: mdl-31822275

RESUMO

BACKGROUND: European Gonococcal Antimicrobial Surveillance Programme (Euro-GASP) antimicrobial resistance (AMR) data are used to inform gonorrhoea treatment guidelines; therefore the data need to be robust and representative. We assessed the extent to which Euro-GASP reflects national measures of the AMR situation for Neisseria gonorrhoeae across the European Union/European Economic Area (EU/EEA). METHODS: We compared data from Euro-GASP with published national gonococcal AMR data from 15 countries for azithromycin, cefixime and ciprofloxacin for the period 2009 to 2013 and performed Poisson regression to identify differences (p < 0.05) between the proportions of resistant isolates. The 2014 Euro-GASP AMR data for each country (n = 19) were weighted to account for differences in the distribution of patient characteristics between Euro-GASP and EU/EEA epidemiological gonorrhoea surveillance data. Data were compared to determine whether estimates of resistance levels differed with regards to the 5% threshold used to assess the clinical utility of first-line gonorrhoea treatments. We assessed the quality of decentralised testing by comparing AMR data for isolates tested both centrally and in the participating laboratories, and by evaluating external quality assessment (EQA) performance. RESULTS: There was no significant difference for azithromycin, cefixime and ciprofloxacin resistance when Euro-GASP country data were compared with data from national reports. Weighting slightly altered the Euro-GASP AMR estimates (by between - 4.7 and 4.7% from the unweighted estimates). Weighting resulted in greater changes in estimates of resistance to azithromycin (from - 9.5 to 2.7%) and ciprofloxacin (from - 14.8 to 17.9%) in countries with low isolate numbers and low completeness of reporting (n = 3). Weighting caused AMR levels to fall below or above the 5% threshold for cefixime or azithromycin, respectively in only two countries. Susceptibility category data submitted from the decentralised Euro-GASP laboratories were concordant with the Euro-GASP data (> 90%). EQA performance was also good; < 5% of the minimum inhibitory concentration (MIC) results differed by > 4-fold from the modal MIC of the EQA isolate. CONCLUSIONS: The overall prevalence of AMR reported by Euro-GASP reflects closely the AMR situation for N. gonorrhoeae in the EU/EEA. Euro-GASP data can be used to provide robust AMR estimates to inform the European guideline for the management of gonorrhoea.


Assuntos
Antibacterianos/farmacologia , Farmacorresistência Bacteriana/efeitos dos fármacos , Neisseria gonorrhoeae/efeitos dos fármacos , Antibacterianos/uso terapêutico , Azitromicina/farmacologia , Azitromicina/uso terapêutico , Cefixima/farmacologia , Cefixima/uso terapêutico , Ciprofloxacino/farmacologia , Ciprofloxacino/uso terapêutico , União Europeia , Gonorreia/diagnóstico , Gonorreia/microbiologia , Humanos , Testes de Sensibilidade Microbiana , Neisseria gonorrhoeae/isolamento & purificação
19.
Chem Pharm Bull (Tokyo) ; 67(12): 1314-1323, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31787658

RESUMO

Condensation of rhodanine (1) with pyrazol-3(2H)-one derivatives (2a-f) gave 5-substituted-2-thioxo-1,3-thiazolidin-4-one derivatives (3a-f). Reaction of compound (1) with 2-arylmethylidene-malononitrile (4a-d) yielded the unexpected derivatives (5a-d). The latter compounds were subjected to cyclization reactions with malononitrile under different basic conditions, hydroxylamine hydrochloride and/or thiourea to furnish the fused thiazole derivatives (6a-d) and (8-10a-d). Coupling of (1) with diazotized aromatic amines (11a-c) in pyridine afforded the arylhydrazones (12a-c). Fusion of latter compounds with malononitrile afforded the thiazolopyridazine derivatives (13a-c). The structures of the newly synthesized compounds were elucidated via spectral data and elemental analyses. The in-vitro cytotoxic activity of compounds (3a-f) against the cell line MCF-7 was evaluated. Also, the synthesized products were investigated for their antibacterial and antifungal activities against six standard organisms including the G+ bacteria, Staphylococcus aureus and Bacillus subtilis, G- bacteria, Escherichia coli and Proteus vulgaris in addition to fungi, Candida albicans and Aspergillus flavus.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Antineoplásicos/farmacologia , Compostos Heterocíclicos/farmacologia , Tiazóis/farmacologia , Antibacterianos/síntese química , Antibacterianos/química , Antifúngicos/síntese química , Antifúngicos/química , Antineoplásicos/síntese química , Antineoplásicos/química , Aspergillus flavus/efeitos dos fármacos , Bacillus subtilis/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Escherichia coli/efeitos dos fármacos , Compostos Heterocíclicos/síntese química , Compostos Heterocíclicos/química , Humanos , Células MCF-7 , Testes de Sensibilidade Microbiana , Proteus vulgaris/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos , Tiazóis/química
20.
Chem Commun (Camb) ; 55(100): 15129-15132, 2019 Dec 12.
Artigo em Inglês | MEDLINE | ID: mdl-31788680

RESUMO

Here, a reaction-based indicator displacement hydrogel assay (RIA) was developed for the detection of hydrogen peroxide (H2O2) via the oxidative release of the optical reporter Alizarin Red S (ARS). In the presence of H2O2, the RIA system displayed potent biofilm inhibition for Methicillin-resistant Staphylococcus aureus (MRSA), as shown through an in vitro assay quantifying antimicrobial efficacy. This work demonstrated the potential of H2O2-responsive hydrogels containing a covalently bound diol-based drug for controlled drug release.


Assuntos
Antraquinonas/química , Antibacterianos/farmacologia , Biofilmes/efeitos dos fármacos , Peróxido de Hidrogênio/química , Staphylococcus aureus Resistente à Meticilina/fisiologia , Antraquinonas/farmacologia , Antibacterianos/química , Escherichia coli/efeitos dos fármacos , Hidrogéis/química , Hidrogéis/farmacologia , Testes de Sensibilidade Microbiana , Pseudomonas aeruginosa/efeitos dos fármacos , Solubilidade
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